38736-78-6Relevant articles and documents
Betulinic acid and its derivatives as anti-angiogenic agents
Mukherjee, Rama,Jaggi, Manu,Rajendran, Praveen,Siddiqui, Mohammad J. A.,Srivastava, Sanjay K.,Vardhan, Anand,Burman, Anand C.
, p. 2181 - 2184 (2004)
Betulinic acid (1) significantly caused cytotoxicity to endothelial cell line ECV304 (IC50 1.26±0.44μg/mL) in a 5-day MTT assay. Novel and more potent derivatives of betulinic acid (2, 4, 6-8) have been synthesized with IC50 less than 0.4μg/mL. The endothelial cell specificity against human tumor cell lines DU145, L132, A549, and PA-1 were determined. Further betulinic acid (1) inhibited TLS formation of ECV304 cells on MatrigelTM by 5.5% while its derivatives caused an inhibition of 13.1-49.2%.
Synthetic Analogues of Betulinic Acid as Potent Inhibitors of PS1/BACE1 Interaction to Reduce Aβ Generation
Zhang, Chenlu,Wang, Xiaoyin,Cui, Jin,Li, Xiaohang,Zhang, Yangming,Wang, Xin,Gu, Haifeng,Li, Wei,Xie, Xin,Zhao, Jian,Pei, Gang,Nan, Fajun
, p. 103 - 112 (2017/02/05)
The lupane-type triterpenoids are endowed with a wide range of biological activities such as antiviral, anti-inflammatory and anticancer activity. We describe here its potential application in Alzheimer's disease (AD) treatment as an inhibitor of PS1/BACE1 interaction. 3-α-Akebonoic acid, which emanated from a high throughput screening (HTS), was discovered to interfere with PS1/BACE1 interaction and reduce amyloid β-protein (Aβ) production. In view of the limited source, we instead used naturally rich betulinic acid (compound 2) as starting material for lead optimization and a focused library of its derivatives was constructed to gain a better understanding of the structure activity relationship (SAR) of triterpenoid-type inhibitor of PS1/BACE1 interaction. Compound 22 was finally chosen as the most potent PS1/BACE1 interaction inhibitor, which reduced Aβ generation effectively.
C-28 AMIDES OF MODIFIED C-3 BETULINIC ACID DERIVATIVES AS HIV MATURATION INHIBITORS
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Page/Page column 198, (2011/12/14)
Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, modified C-3 and C-28 betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors. These compounds are useful for the treatment of HIV and AIDS.
